Effects of thienodiazepine derivatives on human sleep as compared to those of benzodiazepine derivatives

Yoichi Nakazawa, Makoto Kotorii, Masachika Ohshima, Shuichi Horikawa, Hisayuki Tachibana

The effects of new thienodiazepine derivatives, such as clotiazepam and Y-7131, on normal human sleep were investigated on 5 subjects and compared to those of benzodiazepine derivatives, such as diazepam and nitrazepam. REM sleep was significantly decreased only with 2 mg of Y-7131 and rebound elevation of REM sleep did not follow in recovery 1 and 2 nights. By using partial differential REM deprivation which was designed by us, there was also no rebound elevation of REM sleep noted in recovery 2 nights following 2 mg of Y-7131 medication. REM sleep was not suppressed with 15 mg of clotiazepam, 6 mg of diazepam and 10 mg of nitrazepam when compared to the baseline night. With regard to NREM sleep, stage 2 was significantly increased with 15 mg of clotiazepam and 10 mg of nitrazepam, but stage SWS was significantly decreased with 10 mg of nitrazepam.